Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.7.48 extracted from

  • Murakami, E.; Niu, C.; Bao, H.; Micolochick Steuer, H.M.; Whitaker, T.; Nachman, T.; Sofia, M.A.; Wang, P.; Otto, M.J.; Furman, P.A.
    The mechanism of action of beta-D-2-deoxy-2-fluoro-2-C-methylcytidine involves a second metabolic pathway leading to beta-D-2-deoxy-2-fluoro-2-C-methyluridine 5-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase (2008), Antimicrob. Agents Chemother., 52, 458-464.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
S282T the mutation shows reduced sensitivity to 2'-hydroxy-2'-C-methyl nucleosides Hepacivirus C

Inhibitors

Inhibitors Comment Organism Structure
beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-triphosphate PSI-6130-TP, potent inhibitor Hepacivirus C
beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate also named RO2433-TP or PSI-6206, potent inhibitor Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
nucleoside triphosphate + RNAn
-
Hepacivirus C diphosphate + RNAn+1
-
?

Synonyms

Synonyms Comment Organism
NS5B protein
-
Hepacivirus C
RDRP
-
Hepacivirus C
RNA-dependent RNA polymerase
-
Hepacivirus C

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000059
-
beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-triphosphate wild type enzyme, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C
0.00022
-
beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate mutant enzyme S282T, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C
0.00031
-
beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-triphosphate mutant enzyme S282T, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C
0.00042
-
beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate wild type enzyme, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C